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GSK484 | Mixed-mode inhibitor of PADI4
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PADI4
  • IC50:50 nM
  • IC50:250 nM
Mixed-mode inhibitor
Up to 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki, Kii - PADI1: Ki = 108 uM, Kii = 470 uM, PADI2 Ki = 107 uM, Kii = 1350 uM, PADI3 Ki = 2090 uM, Kii = 1230 uM, PADI4 Ki = 6.8 uM, Kii = 65 uM

Selectivity Assessment Description:
Negligible activity in a panel of 50 protein kinases Negligible activity against COX2, MAOB, PDE4 ...

Potency
Cellular
In Vitro

PADI4

Mode of Action: Mixed-mode inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nchembio.1735

Negative Control Compounds

GSK106

Chemical Information

Molecular Formula C27H31N5O3
SMILEs COc1cc(C(=O)N2CC[C@@H](O)[C@@H](N)C2)cc2nc(-c3cc4ccccc4n3CC3CC3)n(C)c12
InChI InChI=1S/C27H31N5O3/c1-30-25-20(11-18(13-24(25)35-2)27(34)31-10-9-23(33)19(28)15-31)29-26(30)22-12-17-5-3-4-6-21(17)32(22)14-16-7-8-16/h3-6,11-13,16,19,23,33H,7-10,14-15,28H2,1-2H3/t19-,23+/m0/s1
Molecular weight 473.24 Da
AlogP 3.147700000000002
HBond acceptors 8
HBond donors 3
Atoms 66

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 18 May 2016)
Cellular Use Rating
(The reviewer did not leave any public comments)
by SERP
(on 20 Dec 2016)
Cellular Use Rating
In Model Organisms
GSK484 is a PADI4-selective in vitro chemical probe. PAD4 is a calcium-dependent enzyme which catalyzes the reaction in which protein arginine residues are converted into citrulline, with the release...
by SERP
(on 7 Jul 2017)
Cellular Use Rating
In Model Organisms
There is solid experimental evidence supporting GSK484 as a PAD4-specific inhibitor in biochemical systems, including nanomolar potencies in fluorescence polarization, ligand-competition, and NH3-release...

Portal Comments

...

(last updated: 7 Nov 2023)

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